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Assay Detail

CHEMBL992476

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at FXR assessed as activation by cell based luciferase transactivation assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Bile acid receptor (CHEMBL2047)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: virtual screening, synthesis, and biological evaluation.
Deng G, Li W, Shen J, Jiang H, Chen K, Liu H.
Bioorg Med Chem Lett (2008) 18 : 5497 -5502
PubMed 18815030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 5.38 5.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL519861 1 5.73
CHEMBL485404 1 5.69
CHEMBL520976 1 5.62
CHEMBL485563 1 5.48
CHEMBL483579 1 5.40
CHEMBL483197 1 5.37
CHEMBL519840 1 5.32
CHEMBL485210 1 5.29
CHEMBL520519 1 5.27
CHEMBL484547 1 5.21
CHEMBL483187 1 5.20
CHEMBL240597 CHENODIOL 4.0 1 5.20
CHEMBL485403 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL519861 EC50 = 1860.0 nM 5.73
CHEMBL485404 EC50 = 2040.0 nM 5.69
CHEMBL520976 EC50 = 2400.0 nM 5.62
CHEMBL485563 EC50 = 3310.0 nM 5.48
CHEMBL483579 EC50 = 3980.0 nM 5.40
CHEMBL483197 EC50 = 4270.0 nM 5.37
CHEMBL519840 EC50 = 4790.0 nM 5.32
CHEMBL485210 EC50 = 5150.0 nM 5.29
CHEMBL520519 EC50 = 5370.0 nM 5.27
CHEMBL484547 EC50 = 6170.0 nM 5.21
CHEMBL483187 EC50 = 6310.0 nM 5.20
CHEMBL240597 CHENODIOL EC50 = 6310.0 nM 5.20
CHEMBL485403 EC50 = 6920.0 nM 5.16